A comparison of the residual effects of zaleplon and zolpidem following administration 5 to 2 h before awakening

• Published in: British journal of clinical pharmacology Vol. 48; no. 3; pp. 367 - 374
• Main Authors: DANJOU, P, PATY, I, FRUNCILLO, R, WORTHINGTON, P, UNRUH, M, CEVALLOS, W, MARTIN, P
• Format: Journal Article
• Language: English
• Published: Oxford, UK Blackwell Science Ltd 01.09.1999; Blackwell Science; Blackwell Science Inc
• Subjects: Acetamides - administration & dosage; Acetamides - adverse effects; Adult; Biological and medical sciences; Double-Blind Method; Drug Administration Schedule; Female; Humans; hypnotic; Hypnotics and Sedatives - administration & dosage; Hypnotics and Sedatives - adverse effects; Hypnotics. Sedatives; Male; Medical sciences; Memory - drug effects; Neuropharmacology; Original; Pharmacology. Drug treatments; Psychology. Psychoanalysis. Psychiatry; Psychomotor Performance - drug effects; Psychopharmacology; Pyridines - administration & dosage; Pyridines - adverse effects; Pyrimidines - administration & dosage; Pyrimidines - adverse effects; residual effects; sedative; zaleplon; Zolpidem; Human; Pharmacokinetic pharmacodynamic relationship; Agonist; Healthy subject; Psychotropic; Memory; Gabaergic agonist; Single dose; Hypnotic; Cognition; Residual effect; Blood; Zaleplon; Blood plasma; Awakening; Reaction time; Zolpidem; Clinical trial; Response latency; Sedative; Pharmacokinetics; Gabaergic receptor A; Comparative study
• ISSN: 0306-5251; 1365-2125
• DOI: 10.1046/j.1365-2125.1999.00024.x

Aims To compare the duration of the residual hypnotic and sedative effects of zaleplon with those of zolpidem and placebo following nocturnal administration at various times before morning awakening. Methods Zaleplon 10 mg, zolpidem 10 mg, or placebo was administered double‐blind to 36 healthy subjects under standardized conditions in a six‐period, incomplete‐block, crossover study. Subjects were gently awakened and given medication at predetermined times 5, 4, 3, or 2 h before morning awakening, which occurred 8 h after bedtime. When the subjects awoke in the morning, a battery of subjective and objective assessments of residual effects of hypnotics was administered. Results No residual effects were demonstrated after zaleplon 10 mg, when administered as little as 2 h before waking, on either subjective or objective assessments, whereas zolpidem 10 mg showed significant residual effects on DSST and memory (immediate and delayed free recall) after administration up to 5 h before waking and choice reaction time, critical flicker fusion threshold and Sternberg memory scanning after administration up to 4 h before waking. Residual effects of zolpidem were apparent in all objective and subjective measurements when the drug was administered later in the night. Conclusions The present results demonstrate that zaleplon at the dose of 10 mg is free of residual hypnotic or sedative effects when administered nocturnally as little as 2 h before waking in normal subjects. In contrast, residual effects of zolpidem are still apparent on objective assessments up to 5 h after nocturnal administration, longer than has been reported from studies involving daytime administration.